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Pharmacology Block 1 > Adrenergics - Catecholamines > Flashcards

Adrenergics - Catecholamines Flashcards

1
Q

Name the Catecholamines (6).

A

Norepinephrine, Epinephrine, Isoproterenol, Dopamine, Dobutamine, Methyldopa

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2
Q

Norepinephrine. What receptors does it work on?

A

a1, a2, b1

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3
Q

Norepinephrine. Agonist or antagonist?

A

Agonist

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4
Q

Norepinephrine. What are its effects?

A

Peripheral vasoconstriction (a1 receptor), Increase BP (B1 and A1 receptor), no increase in HR b/c vagal reflex to decrease HR in presence of increased TPR and BP

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5
Q

Norepinephrine. Therapeutic uses (2).

A

Vasoconstrictor in intensive care situations

Elevate blood pressure during reduced sympathetic tone -> anesthesia, or neural injury

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6
Q

Epinepherine. What receptors does it work on?

A

A1, A2, B1, B2

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7
Q

Epinepherine. Agonist or antagonist?

A

Agonist

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8
Q

Epinephrine. What are its effects? CV, Respiratory, and Metabolic

A

CV - Increase HR, no net change in BP, slight decrease in PVR
Respiratory - Bronchodilation (B2 receptor)
Metabolic - gluconeogenesis, glycogenolysis, lipolysis, inhibit insulin release (b2 receptors)

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9
Q

Epinephrine. Explain the CV effects of this drug.

A

Increase in HR b/c of increase in contractile force and AV node conduction b/c direct stimulation of B1 Receptor.
No change in BP b/c increase in systolic but decrease in diastolic BP (b2 receptor)
Decrease in TVR b/c dilation of skeletal muscles via B2 receptor even with construction of other vessels via A receptors.

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10
Q

How is epinephrine administered?

A

Parentrally

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11
Q

Epinephrine. What receptor is most acted on?

A

B2

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12
Q

Explain the dose dependent CV effects of Epinephrine.

A

Moderate dose -> vasodilation b/c direct action of b2 receptors on skeletal muscle vessels -> dilation
Higher dose -> vasoconstriction b/c b receptors are full so drug starts binding to a receptors causing vasoconstriction of all vessels

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13
Q

Epinephrine. Therapeutic uses (4)

A

Rapid relief of hypersensitivity
Opthalmic -> pupil dilation
With local anesthetics (vasoconstriction) to increase time of action
Bradyarrhythmias -> restore contractility/rhythm in pts with cardiac arrest

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14
Q

Isoproterenol. What receptors does it bind?

A

B1, B2

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15
Q

Isoproterenol. Agonist or antagonist?

A

Agonist

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16
Q

Isoproterenol. What are its effects. CV, Respiratory

A

CV - Decrease BP and TVR (b/c b2 receptor and vasodilation), increase HR b/c direct stimulation of B1 receptor AND feedback from dec. BP
Respiratory - bronchodilation

17
Q

What are the therapeutic uses of isoproterenol?

A

In emergencies to stimulation HR during bradycardia or heart block.

18
Q

Is dopamine an antagonist or agonist?

A

Agonist

19
Q

What receptors does dopamine act one?

A

DA1, A1, B1

20
Q

What are the CV effects of dopamine - low dose?, medium dose?, high dose?

A

Low dose - 0.5ug/kg -> acts in DA1 receptor to increase renal blood flow by dilating renal vasculature
Medium dose - 5-10ug/kg -> acts on B1 receptor to increase HR and contractility (increase CO)
High Dose - 10-20ug/kg -> acts on A1 receptor, vasoconstriction and increase TPR

21
Q

What are the therapeutic uses for dopamine?

A

severe decompensated heart failure, shock

22
Q

Is dobutamine an agonist or antagonist?

A

Mixed b/c racemic

23
Q

What receptors does dobutamine act on? (-, +, Racemic)

A

(-) -> a1 agonist, b agonist
(+) -> a1 antagonist, b agonist
Racemic -> b1 agonist

24
Q

What are the therapeutic effects of dobutamine?

A

Increase HR and contractility, minimal change in BP and TPR

25
Q

What are the therapeutic uses of dobutamine? (2)

A

Short term treatment of cardiac decompensation

Cardiac stress testing -> stress the heart to do the testing of pt is unable to exercise

26
Q

What is significantly unique about methyldopa?

A

Orally active prodrug

27
Q

What receptor does methyldopa act on?

A

A2

28
Q

Is methyldopa an agonist or antagonist?

A

agonist

29
Q

What are the effects of methyldopa?

A

decrease peripheral R, decrease HR, decrease CO

30
Q

What is the major therapeutic use of methyldopa?

A

HTN, especially gestational b/c been proven to be safe for baby

31
Q

What are the side effects of methyldopa? (4)

A

Sedation, dry mouth, edema, rebound HTN with sudden discontinuation

32
Q

Explain the mechanism of action of methyldopa?

A

a-methyldopa -> CNS nerve cell ->decarboxylated by acid decarbozylase now is a-methyldopamine -> to storage granules via transporter -> converted to a-methylnorepinepherine by dopamine hydrozylase -> released instead of NE and acts on a2 receptors IN CNS

33
Q

What prevents methyldopa deradation by MAO? What is the significance of that clinically?

A

alpha methyl group prevents degradation -> reason it can be given orally, long half life

Pharmacology Block 1 (8 decks)

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